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WRW4

WRW4, Formyl Peptide Receptor-Like 1 (FPRL1) Antagonist
A Potent Antagonist of FPR2 and FPR3 G-Protein Coupled Receptors
Cat #: GPW-110
Alternative Name WRW4, Formyl Peptide Receptor-Like 1 (FPRL1) Antagonist
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 1104.3 Da.
    Purity: >98% (HPLC)
    Effective concentration 1 nM - 10 μM.
    Sequence WRWWWW.
    Modifications Trp6 - C-terminal amidation.
    Molecular formula C61H65N15O6.
    CAS No.: 878557-55-2.
    Activity WRW4 is a selective and potent antagonist of the formyl peptide receptor (FPR2)1.
    References-Activity
    1. Bae, Y.S. et al. (2004) J. Immunol. 173, 607.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DDW only for stock solutions of up to 1mM (further dilutions of stock solution can be done in any physiological buffer). Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs WRW4 blocks Ca2+ transients in differentiated HL-60 cells, generated by MMK1 application.
      Alomone Labs WRW4 blocks Ca2+ transients in differentiated HL-60 cells, generated by MMK1 application.
      Cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following application (indicated by arrow) of 1µM MMK1 (#GPM-120). 30min pre-incubation with various concentrations of WRW4 (#GPW-110) resulted in a dose-dependent inhibition of FPR2 activation. A. Normalized fluorescence levels before and after application (indicated by an arrow) of control saline solution (black) or of 1µM MMK1 in cells pre-incubated with 0 µM (red), 0.25 µM (green), 1 µM (purple) and 5 µM (blue) WRW4. B. Inhibition of FPR2 activation plotted against WRW4 concentrations.
    References - Scientific background
    1. Ye, R.D. et al. (2009) Pharmacol. Rev. 61, 119.
    2. Le, Y. et al. (2002) Trends Immunol. 23, 541.
    3. Bae, Y.S. et al. (2004) J. Immunol. 173, 607.
    4. Shin, E.H. et al. (2006) Biochem. Biophys. Res. Commun. 341, 1317.
    5. Lee, H.Y. et al. (2010) Exp. Mol. Med. 42, 302.
    6. See Applications for Anti-Human FPR2/ALX (extracellular) Antibody.
    Scientific background

    Chemotactic factors from both Gram-positive and Gram-negative bacteria are short peptides with N-formyl methionine at the N-terminus (extensively reviewed in reference 1). These peptides are released from bacteria during infection and activate formyl peptide receptors (FPR), members of the G-protein coupled receptor (GPCR) superfamily. In humans, the FPR family consists mainly of three receptors, FPR1FPR2/ALX (formerly FPRL1), and FPR3 (formerly FPRL2) which all couple to the Gi subtype of G-proteins and ultimately lead to the activation of phospholipase C and intracellular Ca2+ increase1,2.

    WRW4 is a selective and potent antagonist of the Formyl peptide receptors (FPR2 and FPR3)3,4, which was identified by screening hexapeptide libraries that inhibit the binding of the FPR2 agonist WKYMVm to its specific receptor, in RBL-2H3 cells3. In human umbilical vein endothelial cells, WRW4 (10 mM), inhibited CCL2 production, which was stimulated by serum amyloid A5.

    FPR2 is expressed in the promyelocytic leukemia cell line HL-60 as well as in the chronic myelogenous leukemia cell line K5626. In human neutrophils, 10 µM WRW4 blocked the specific FPR2 agonist (MMK1) induced Ca2+ influx. In addition, at the same concentration WRW4 blocked Ca2+ influxes, generated by stimulation with the Alzheimer’s diseases Amiloide β42 peptide, by lipoxin A4 and by fMLF3.

    Net Peptide Content: 100%
    Last update: 16/08/2020

    WRW4 (#GPW-110) is a highly pure, synthetic, and biologically active peptide.

    For research purposes only, not for human use

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    Scientific Background

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